EP4033921A1 - Composition d'un complément alimentaire et/ou d'un additif nutritionnel pour aliments, forme posologique unitaire de ladite composition, et leur utilisation pour l'amélioration de la qualité de performance visuelle, y compris la sensibilité de contraste chez des personnes ayant besoin d'une telle amélioration, y compris des personnes souffrant d'au moins une maladie oculaire, en particulier le corps flottant du vitré - Google Patents

Composition d'un complément alimentaire et/ou d'un additif nutritionnel pour aliments, forme posologique unitaire de ladite composition, et leur utilisation pour l'amélioration de la qualité de performance visuelle, y compris la sensibilité de contraste chez des personnes ayant besoin d'une telle amélioration, y compris des personnes souffrant d'au moins une maladie oculaire, en particulier le corps flottant du vitré

Info

Publication number
EP4033921A1
EP4033921A1 EP20797888.3A EP20797888A EP4033921A1 EP 4033921 A1 EP4033921 A1 EP 4033921A1 EP 20797888 A EP20797888 A EP 20797888A EP 4033921 A1 EP4033921 A1 EP 4033921A1
Authority
EP
European Patent Office
Prior art keywords
composition
extract
dosage form
persons
floaters
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
EP20797888.3A
Other languages
German (de)
English (en)
Inventor
John Nolan
Emmanuel ANKAMAH
Maciej OSEKA
Robert KUCHLING
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Ebiga Vision GmbH
Maciej Oseka 4eyez
Original Assignee
Ebiga Vision GmbH
Maciej Oseka 4eyez
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Ebiga Vision GmbH, Maciej Oseka 4eyez filed Critical Ebiga Vision GmbH
Publication of EP4033921A1 publication Critical patent/EP4033921A1/fr
Pending legal-status Critical Current

Links

Classifications

    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
    • A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
    • A23L33/17—Amino acids, peptides or proteins
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
    • A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
    • A23L33/17—Amino acids, peptides or proteins
    • A23L33/175—Amino acids
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
    • A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
    • A23L33/105—Plant extracts, their artificial duplicates or their derivatives
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
    • A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
    • A23L33/15—Vitamins
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
    • A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
    • A23L33/16—Inorganic salts, minerals or trace elements
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
    • A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/365—Lactones
    • A61K31/375—Ascorbic acid, i.e. vitamin C; Salts thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00—Medicinal preparations containing inorganic active ingredients
    • A61K33/24—Heavy metals; Compounds thereof
    • A61K33/30—Zinc; Compounds thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/75—Rutaceae (Rue family)
    • A61K36/752—Citrus, e.g. lime, orange or lemon
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/87—Vitaceae or Ampelidaceae (Vine or Grape family), e.g. wine grapes, muscadine or peppervine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
    • A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
    • A23V2250/00—Food ingredients
    • A23V2250/02—Acid
    • A23V2250/06—Amino acid
    • A23V2250/063—Lysine
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
    • A23V2250/00—Food ingredients
    • A23V2250/15—Inorganic Compounds
    • A23V2250/156—Mineral combination
    • A23V2250/1642—Zinc
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
    • A23V2250/00—Food ingredients
    • A23V2250/20—Natural extracts
    • A23V2250/21—Plant extracts
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
    • A23V2250/00—Food ingredients
    • A23V2250/70—Vitamins
    • A23V2250/708—Vitamin C
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

Definitions

  • the invention concerns a composition of a dietary supplement and/or a nutritional additive for food comprising as active substances L-lysine, vitamin C, zinc, grape extract and bitter orange extract in therapeutically effective quantities.
  • the subject-matter of the invention is also a unitary dosage form comprising said composition of the dietary supplement and/or the nutritional additive for food.
  • the subject-matter of the invention is, furthermore, a use of the above-mentioned composition and unitary dosage form for improvement of the quality of visual performance including contrast sensitivity in persons in need of such an improvement and for improvement of the quality of life of these persons, including persons, which were diagnosed to suffer from at least one eye disease, and in particular from vitreous floaters.
  • Patent specification EP 2883544 B1 informs that the oral application of the dietary supplement in the form of a preparation comprising lutein, zeaxanthin along with other nutritional ingredients supports the increase of the optical density of the macular pigment (MPOD), may protect the eye retina from the negative impact of light radiation, and may inhibit the development of the age-related macular disease, AMD.
  • MPOD optical density of the macular pigment
  • the oral application of the dietary supplement comprising various nutritional ingredients, among others zeaxanthin, vitamin C, vitamin E and zinc, has a positive impact on patients suffering from AMD, and in particular on those patients which are in the so-called "geographic atrophy” stage of this disease or a comparable stage of another eye disorder.
  • Patent document EP 2433640 A1 teaches that lutein and zeaxanthin along with the superoxide dismutase (SOD) protect eye photoreceptors against the damaging impact of the ultraviolet radiation.
  • SOD superoxide dismutase
  • Vitreous floaters are another of the above-mentioned eye diseases of a growing significance in recent years.
  • This eye disorder affects the vitreous body of the eye and leads to deepening degeneration in this eye organ.
  • the disease can be extremely bothersome for patients, causing significant difficulties in everyday life. If left untreated, it progresses, serves as a precursor for the development of other accompanying eye diseases, and causes ever-increasing disability of the patients.
  • Understanding the perspective of the patients suffering from vitreous floaters and the impact of the symptoms of the disease on their assessment of the quality of life is one of issues recently addressed in medical practice. This is because it has been proven that disease symptoms reported by the patients are particularly essential for clinical trials (Guyatt, G.H., C. Bombardier, and P.X. Tugwell, "Measuring disease-specific quality of life in clinical trials", CMAJ: Canadian Medical Association Journal, 1986. 134(8): p. 889).
  • the posterior segment of the human eye houses a uniformly transparent gel of a complex structure, an extracellular matrix made up in 99% of water and collagen, proteins and hyaluronic acid, forming an eye organ called the vitreous body.
  • the total volume of the human vitreous body is about 4 ml.
  • a small number of cells, mainly hyalocytes, astrocytes and glial cells physiologically present in the vitreous body, are located in the area of the cortex of the vitreous body.
  • the vitreous body constitutes structural support to the eyeball occupying it up to 3 ⁇ 4. Thanks to its transparency it allows unhindered transmission of light.
  • the vitreous body conditions the lucidity of the interior of the eyeball, it is responsible for the shape of the eyeball and maintains the correct intraocular pressure.
  • collagen fibres get dissociated from hyaluronic acid and aggregated as clumps, forming watery spaces or lacunae containing hyaluronic acid and water.
  • vitreous floaters develop mechanisms of vitreous floaters include connective tissue disorders, which consist in the combination of collagen fibre proteins of the vitreous body under glycation and oxidative stress, and increased proteolytic activity of enzymes in the vitreous body (Bishop, P.N., et al., "Age-related changes on the surface of vitreous collagen fibrils", Investigative ophthalmology & visual science, 2004. 45(4): p. 1041-1046) (Harocopos, G.J., et al., "Importance of vitreous liquefaction in age-related cataract", Investigative ophthalmology & visual science, 2004. 45(1): p. 77-85).
  • Bundles of clustered collagen fibres form moveable turbidities called vitreous floaters, which are perceived by the patients as “flies”, “webs”, “clouds” or “shadows” within the visual field, the severity of which usually gets intensified when moving the head or eyes.
  • the severity of vitreous floaters depends also on their size and density, distance from the retina and the visual axis, and the width of the pupil. Vitreous floaters disperse light causing blurred vision or haze and increase sensitivity to glare.
  • Vitreous floaters appearing near or within the optical axis of the eye impair vision and, as a consequence, impact negatively on important daily life activities, such as reading, working on a computer, watching objects particularly in the open air in good light conditions, driving a car, and near-work activities.
  • both the quality of visual performance is reduced, as well as the quality of life of persons suffering from the degeneration of the vitreous body (Huang, L.C., et al., Erratum: “Vitreous Floaters and Vision: Current Concepts and Management Paradigms”, in Vitreous, 2014, Springer p. E1-E2) (Yonemoto, J., et al., “The age of onset of posterior vitreous detachment”.
  • Vitreous floaters disturb the quality of vision and negatively impact the quality of life. Patients have described vitreous floaters as a nuisance which decrease their life comfort (Cipolletta, S., A. Beccarello, and A. Galan, “A psychological perspective of eye floaters”, Qualitative health research, 2012. 22(11): p. 1547-1558) (Zou, H., et al., “The impact of persistent visually disabling vitreous floaters on health status utility values”, Quality of Life Research, 2013. 22(6): p. 1507-1514).
  • vitreous floaters decrease life comfort, to a degree comparable to AMD, diabetic retinopathy, glaucoma, a light version of angina pectoris, a light stroke, colon cancer and asymptomatic HIV.
  • the patients are willing to trade 1,1 years of every 10 years of their remaining life to get rid of the vitreous floaters (Wagle, A.M., et al., “Utility values associated with vitreous floaters”, American journal of ophthalmology, 2011. 152(1): p. 60-65. e1.).
  • a surgical treatment which consists in removing part or whole vitreous body may have complications, such as retinal detachment, cataract, glaucoma, haemorrhage to the chamber of the vitreous body and macula oedema.
  • Other treatment methods include laser vitreolysis performed with a neodymium-doped yttrium aluminum laser (Nd-YAG) and administering eye drops, but their effectiveness and safety have not been unequivocally proven (SA, A. and A.
  • compositions of dietary supplements which comprise combinations of various nutritional ingredients, for use in eye diseases.
  • compositions of dietary supplements meant for the patients with vitreous floaters with proven evident and direct impact on the objective and subjective assessment of the quality of visual performance in these patients.
  • a composition of a dietary supplement which would ensure complex support of eye functions by improving the subjective assessment of the quality of life in persons suffering from eye diseases or persons jeopardized with the possible development of eye diseases, and by improving the ability to see.
  • the inventors of the present invention have also noticed the need to develop a composition of a dietary supplement meant for persons suffering from eye diseases, and in particular for persons suffering from vitreous floaters, to treat these diseases, to slow down their development or to inhibit them, and to prevent their appearance.
  • vitreous floaters are nowadays a very common issue
  • the inventors of the present invention have launched research aiming at development of a composition of a dietary supplement and its dosage regime which would ensure improving the subjective assessment of the quality of life in persons with eye diseases, and in particular in persons with vitreous floaters, as well as improving the quality of visual performance in these persons measured by objective study methods.
  • composition of the dietary supplement according to the present invention aims were reached with the composition of the dietary supplement according to the present invention, whereas it has unexpectedly turned out that simultaneous inclusion in the composition of L-lysine, vitamin C, zinc, the grape extract and the bitter orange extract significantly improves the subjective assessment of the quality of life in persons suffering from vitreous floaters, and the objective assessment of the quality of visual performance measured with the contrast sensitivity.
  • composition of a dietary supplement and/or nutritional additive for food according to the present invention contains as active substances L-lysine, vitamin C, zinc, grape extract and bitter orange extract in therapeutically effective quantities, and potentially at least one excipient.
  • percentages of individual active substances of the composition relative to a sum of percentages of all active substances are: a) about 50% by weight of L-lysine, b) about 15% by weight of vitamin C, c) about 2% by weight of zinc, d) about 10% by weight of the grape extract, e) about 23% by weight of the bitter orange extract, with all percentages of the individual active substances adding up to 100% by weight of all active substances.
  • the composition contains: a) from about 125 g to about 250 mg of L-lysine, b) from about 40 mg to about 80 mg of vitamin C, c) from about 5 mg to about 10 mg of zinc, d) from about 25 mg to about 50 mg of the grape extract, e) from about 60 mg to about 120 mg of the bitter orange extract.
  • the ingredients of the composition constitute a mixture.
  • the grape extract and/or the bitter orange extract is selected from the group comprising the extract from fruit seeds, the extract from grape pulp, the extract from grape skin, the extract from blossoms of these plants, or their combinations.
  • the grape extract is a grape extract of the Vitis Vinifera species and/or the bitter orange extract is a bitter orange extract of the Citrus Aurantium species, preferably, both extracts DER 100:1.
  • the excipient is a substance nutritionally permitted and is selected from the group comprising at least a vehicle agent, a bulking agent, a binding agent, a disintegrant, a surfactant, a lubricant, an anti-caking agent, an acidity regulator, an antioxidant, a synthetic and/or natural colourant, a colour retaining substance, an emulsifier, a sweetener, an aromatizing agent, a flavouring agent, a flavour enhancer, a preservative, a stabilizing agent, a solvent and a diluent, or their mixtures.
  • the composition has a form of any formulation adequate for oral application such as a powder or a granulate or a liquid or a gel.
  • the composition is applied in a preferred dose, frequency and form for a period of at least 2 months, preferably for a period of at least 3 months and more preferably for a period of at least 6 months.
  • a unitary dosage form according to the present invention contains the composition of the dietary supplement and/or nutritional additive for food according to the present invention.
  • the unitary dosage form contains a daily dose of the active substances of the present composition.
  • the unitary dosage form has a form selected from the group comprising at least a capsule, a tablet, a sachet, a “stick-type” sachet and an ampoule, including any of these forms ensuring a prolonged release of the active substances of the composition in time of at least 3 hours after consumption.
  • a composition of the dietary supplement and/or nutritional additive for food and a unitary dosage form, according to the present invention, are characterized in that they are meant for use with the objective to improve quality of visual performance including contrast sensitivity in persons in need of such an improvement and to improve quality of life of these persons.
  • a composition of a dietary supplement and/or nutritional additive for food and a unitary dosage form according to the present invention are characterized in that they are meant for use in treating eye diseases and/or slowing down and/or inhibiting their development and/or preventing them.
  • the composition and the unitary dosage form according to the present invention are characterized in that they are meant for the use in persons suffering from vitreous floaters.
  • the use of the composition and the unitary dosage form according to the present invention is characterized in that it is meant for persons suffering from vitreous floaters.
  • the extract may be condensed up to the state when the solvent is completely removed.
  • Suitable extracts are available on the market, but they may be also produced with methods known in the field of plant extracts preparation.
  • the grape extract is a grape extract of Vitis Vinifera species DER 100:1 and the bitter orange extract is a bitter orange extract of Citrus Aurantium species DER 100:1.
  • DER means drug extract ratio, which is a ratio of the quantity of the plant raw material used for producing the plant extract to the quantity of the obtained plant extract.
  • excipient is to be understood widely as one substance or a greater number of substances or their mixtures, which are usually used for producing typical compositions of dietary supplements and/or nutritional additives for food, also including beverages, and/or for producing typical pharmaceutical compositions.
  • the excipient may be, thus, any substance nutritionally acceptable which is, however, as well as its content in the composition of the dietary supplement according to the present invention, selected respectively to the active substance content in that composition and to the formulation of that composition and to the unitary dosage form according to the present invention, as well as respectively to production methods of the composition, the formulation and the unitary dosage form according to the present invention.
  • the choice of the suitable excipients constitutes knowledge of an average person skilled in the art of formulating compositions of dietary supplements and/or pharmaceutical compositions.
  • composition of the dietary supplement and/or nutritional additive for food according to the present invention may be the formulation in any form suitable for consumption and adequate for oral administration by a human.
  • the composition of the dietary supplement and/or nutritional additive for food according to the present invention is the formulation in the form of a powder or a granulate.
  • the ingredients of the composition that is the active substances and the excipients if they are contained in the composition, are subjected to normal mixing or granulation with techniques known to the person skilled in the art of pharmacy.
  • the composition of the dietary supplement and/or nutritional additive for food according to the present invention may be the formulation in any form suitable for drinking such as liquid or gel.
  • compositions for oral administration or produced from the composition according to the present invention which have the form of a powder or a granulate or a liquid or a gel, are subsequently used for producing the unitary dosage form.
  • compositions according to the present invention respectively contained and/or closed in a casing for the unitary dosage form such as a capsule, a tablet, a sachet, a “stick-type” sachet or an ampoule, may, preferably, require to be stirred in water or a beverage or another liquid before consumption according to the needs of a patient or according to her/his taste preferences.
  • Some of the active substances of the composition may be given the form of a powder or a granulate or a liquid or a gel by grinding or granulation or liquefaction or gelling, and then be closed, for instance, in microcapsules, before their inclusion into the final formulation form ready for being consumed and before producing the unitary dosage form of the composition according to the present invention.
  • the unitary dosage form of the composition of the dietary supplement and/or nutritional additive for food according to the present invention contains a daily dose of the active substances of the present composition.
  • a unitary dosage form according to the present invention filled with the composition according to the present invention allows the use of the unitary dosage form once a day and simultaneously obtaining the desired therapeutic effect.
  • the unitary dosage form in the context of the present invention is meant for oral administration. Therefore, preferably, the unitary dosage form has a form selected from the group comprising at least a capsule, a tablet, a sachet, a “stick-type” sachet and an ampoule, including any of these forms ensuring a prolonged release of the active substances of the composition in time of at least 3 hours after consumption.
  • the production of the unitary dosage forms according to the present invention with the composition of the dietary supplement and/or nutritional additive for food according to the present invention are technological operations known in the pharmaceutical technology and are realized using standard instruments.
  • the selection of the active substances in the composition of the dietary supplement and/or nutritional additive for food according to the present invention was made by the inventors basing on the knowledge about pathomechanisms of the development of vitreous floaters and potential substances inhibiting these mechanisms. Substances having properties required in the present invention were selected basing on the evidence from in vitro studies as well as the knowledge of the impact of these substances on the physiological functions of other organs in the human body.
  • the active substances of the composition have been selected accordingly - those which decrease intravitreal oxidative stress, which means that they have antioxidant properties and neutralize free radicals in aqueous environment, that is vitamin C and zinc, as well as substances which strongly hamper the glycation of collagen fibres and decrease the activity of enzymes responsible for collagen disintegration, that is L-lysine, the grape extract and the bitter orange extract.
  • L-lysine is an essential amino acid, which needs to be obtained from food as the human organism cannot produce it, and which among others supports the creation of collagen. L- lysine is the free form of this essential amino acid and is absorbed directly into the bloodstream.
  • oligomeric proanthocyanidin complexes or oligomeric proanthocyanidins (OPC), which are commonly known as "super antioxidants” due to their strong antioxidant properties and properties of hampering activity of proteases breaking collagen fibres.
  • OPC oligomeric proanthocyanidins
  • Proanthocyanidins are known also as bioflavonoids and contain hesperidin in high concentrations, which has, apart from antioxidant properties, also anti-inflammatory and protective properties on blood vessels, thereby improving the state of capillaries as well as decreasing their permeability.
  • composition according to the present invention for the grape extract a grape extract of the Vitis Vinifera species was chosen and for the bitter orange extract a bitter orange (OPC) extract of the Citrus Aurantium species.
  • OPC bitter orange
  • compositions according to the present invention in the form of the powder or the granulate or the liquid or the gel subsequently serve to produce the unitary dosage form.
  • various forms of the formulation of the composition according to the present invention are placed in the casing or the sheath to obtain the unitary dosage form in the form of the capsule for instance.
  • the inventors matched the percentages by weight of the individual active substances relative to the sum of the percentages by weight of all four active substances, taking into account the guidelines concerning the quantity of the individual active substances for dietary supplements and doses of dietary supplements, which quantities have to reflect the content of the individual active substances in natural or food products and cannot exceed the acceptable quantities and doses for a dietary supplement.
  • the powdered active substances in the respective percentages by weight were used to prepare the mixture, which was closed in the unitary dosage form in the form of the capsule.
  • One capsule contained 125 mg of L-lysine, 40 mg of vitamin C, 5 mg of zinc, 25 mg of the grape extract of the Vitis Vinifera species DER 100:1 and 60 mg of the bitter orange extract of the Citrus Aurantium species DER 100:1.
  • Such capsules were administered to persons from the active group in the course of the studies conducted as described below in the preferred embodiment of the present invention.
  • the unitary dosage forms may contain also other doses of the composition according to the present invention, including the daily dose of the active substances contained in the composition, subject to requirements concerning dietary supplements.
  • the present invention foresees the use of different formulation forms adequate for oral application for the composition according to the present invention and different forms of the unitary dosage form, as well as different doses of the active substances of the present composition in the unitary dosage form. Thanks to that, after the doctor has determined a therapeutically effective dose of the composition according to the present invention for each patient at a specific stage of therapy or prevention, the patient will be able to apply the unitary dosage form suitable for her/him with the suitable dose of the composition.
  • small doses of the composition according to the present invention may be applied preferably in the beginning and the dosage may be gradually increased up to the point when a clear positive impact is observed on the subjective assessment of the quality of life given by the patient with a given eye disease and/or on the objective parameters of the quality of visual performance in this patient.
  • high doses of the composition according to the present invention could be administered initially and gradually decreased up to the point when a subjective or objective improvement in visual performance is achieved for the given patient.
  • the dietary supplementation period required to evoke a measurable improvement of the subjective assessment of the quality of life and of the objective assessment of the ability to see in persons with vitreous floaters depends on a number of factors, including the state of the development of the disease and the state of the general health of the patients before the commencement of the dietary supplementation as well as on the administered daily dose of the composition according to the present invention.
  • the studies conducted show that to elicit an improvement, dietary supplementation with the composition according to the present invention is required for at least 8 weeks, and more preferably for at least 3 to 6 months before the contrast sensitivity is measured following the supplementation.
  • the inventors of the present invention have attempted to study the effects of the supplementation with the composition according to the present invention on the subjective assessment of the quality of life changes in patients with vitreous floaters and on the changes in objective visual performance parameters in these persons, especially changes in sensitivity to contrast.
  • the visual performance quality parameters are objective parameters which assess the ability to see because they are tested with objective methods of assessment on special medical devices.
  • a non-standard questionnaire was prepared for each individual patient to complete pre and post supplementation with the composition according to the present invention. The content of the questionnaire has been presented below towards the end of the present description.
  • the questionnaire allowed study participants to classify their assessment of the feelings regarding the quality of visual performance since it served to capture the subjective responses of the patients with vitreous floaters regarding the severity of the disease and its impact on their daily functioning.
  • Contrast is the difference in visual properties which makes an object or its pictorial representation discernable from other objects and the background. In the visual perception of the real world, the contrast is determined by the difference in colour and the brightness of the object and other objects within the same visual field. Contrast sensitivity is a measurement of the sensitivity of an individual towards changes in contrast and is indispensable for detecting an object as being separate from the background.
  • the present invention provides the composition of nutritional substances for oral application, which positively affects the quality of eye-sight and sensitivity to contrast in persons with vitreous floaters.
  • Table 1 presents changes in the frequency of reported disturbances caused by the vitreous floaters in the control group and the active group after 6 months of supplementation
  • Table 2 presents changes in the assessment of the impact of vitreous floaters on the daily life in the control group and the active group after 6 months of supplementation
  • Table 3 presents the comparison of the changes in visual functions in the active and control groups before and after supplementation.
  • the active group received the composition according to the present invention formulated as the mixture from the powdered active substances in respective percentages by weight and closed in the unitary dosage form in the form of the capsule.
  • One capsule contained 125 mg of L-lysine, 40 mg of vitamin C, 5 mg of zinc, 25 mg of the Vitis Vinifera grape extract DER 100:1 and 60 mg of the Citrus Aurantium bitter orange extract DER 100:1.
  • the patients from the active group consumed the composition according to the present invention in the amount of one capsule a day for 6 months.
  • the control group received a placebo capsule containing microcrystalline cellulose which had similar shape and colour to the capsule containing the tested composition according to the present invention.
  • the contrast sensitivity parameter (Multiquity LogCS Score), which is an objective assessment parameter of the quality of visual performance, was measured for each patient before and after supplementation, using the MiQ Contrast 256 test, Smolarek- Kasprzak, P., et al., “Measuring visual function using the MultiQuity system: Comparison with an established device”, Journal of ophthalmology, 2014. Binocular contrast thresholds (%) in photopic and mesopic conditions were measured with the Acuity-plus test from the Advanced Vision and Optometric Test (AVOT). Retinal function (rods and cones) was assessed with the Flicker-plus test from the AVOT suite, which employs a 15Hz flicker stimulus. Macular Pigment (MP) was measured with the use of the multi colour Heidelberg Spectralis HRA + OCT test from Heidelberg Engineering GmbH, Heidelberg, Germany.
  • vitreous floaters The impact of vitreous floaters on certain activities: reading small letters (drugs or cosmetics information leaflets), reading newspapers or books, driving a car during the day, using a computer or a mobile phone, watching TV was assessed before the commencement of the study at the baseline visit and after the end of the study at the final visit by subjects responding with either “Yes” or “No” to each activity.
  • a “Yes” response for a certain activity meant disturbances caused by vitreous floaters during this activity.
  • a positive response was scored 1, a negative 0.
  • An overall activity score was calculated by summing up and averaging the individual activity scores reported by each participant of the study. The median overall activity score was determined for each tested group at the baseline and final visits, compared between the groups and within the groups pre and post supplementation.
  • the active group was stratified by age, sex and posterior vitreous detachment (PVD) status.
  • PVD posterior vitreous detachment
  • IQR median score
  • PVD in this case referred to the subjects with complete posterior vitreous detachment, which was observed in the biomicroscopy with the aid of the optical coherent tomography (OCT) and in the slit lamp.
  • IQR median score
  • the questionnaire should be assessed by a clinician.
  • the questionnaire is adapted to assess the functional disturbances of vitreous floaters.
  • Theme 1 Eyes with vitreous floaters
  • Theme 2 The eye suffering from greater floater disturbances Question: Which of your eyes bothers you more: the right or the left?
  • Theme 3 Frequency of floater disturbances during the day Question: When during the day are the floaters most bothersome for you: in the morning, afternoon, evening or never?
  • Theme 4 Impact of vitreous floaters on daily life
  • My condition has been stable and I have not been bothered by my floaters My floaters appear occasionally and are moderately bothersome My floaters appear all the time and are consistently bothersome
  • the supplementation with the composition according to the present invention improves the subjective assessment of the quality of life of persons suffering from vitreous floaters. Simultaneously, unexpectedly for the inventors, after 6 months of conducting studies, there has been observed the significant improvement of the contrast sensitivity in the active group which received the composition of the dietary supplement according to the present invention and a lack of a relevant change in the control group which was given the placebo. The significant improvement of the contrast sensitivity in the active group which received the composition of the dietary supplement according to the present invention was statistically relevant in comparison with the group which did not receive this composition.
  • the performance of the composition of the dietary supplement is not affected by age, sex and the presence and development stage of posterior vitreous detachment (PVD). During the 6-month supplementation period with the composition according to the present invention, persons from the active group did not report any side-effects of the studied composition.
  • PVD posterior vitreous detachment
  • the inventors unexpectedly observed that the consumption of the composition of the dietary supplement and/or nutritional additive for food according to the present invention significantly improves the subjective assessment of the quality of life in persons suffering from vitreous floaters.
  • the present invention provides the composition of nutritional substances for oral administration, which positively impacts the quality of vision and contrast sensitivity in persons suffering from vitreous floaters. Simultaneously, basing on the general knowledge on and experience in pathomechanisms, the course and development of various eye diseases, and the knowledge on the properties of the active substances used in the composition according to the present invention, and basing on the studies conducted for the purpose of the present invention and described above, which related to persons suffering from vitreous floaters, it is claimed that the developed composition and the unitary dosage form according to the present invention are suitable to provide a similar positive therapeutic effect and be used also in treating other different eye diseases and/or slowing down their development and/or inhibiting their development and/or preventing them, as well as, more generally, to be used with the aim to improve the quality of visual performance including contrast sensitivity in all persons in need of such an improvement, and with the aim to improve the quality of life of these persons.

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Abstract

L'invention concerne une composition d'un complément alimentaire et/ou d'un additif nutritionnel pour des aliments, une forme posologique unitaire de ladite composition, et leur utilisation pour l'amélioration de la qualité de performance visuelle, y compris la sensibilité de contraste chez des personnes ayant besoin d'une telle amélioration, y compris des personnes souffrant d'au moins une maladie oculaire, en particulier le corps flottant du vitré. La composition du complément alimentaire et/ou de l'additif nutritionnel pour des aliments selon l'invention comprend, en tant que substances actives, la L-lysine, la vitamine C, le zinc, un extrait de raisin et un extrait d'orange amère en quantités thérapeutiquement efficaces, et éventuellement au moins un excipient. Dans le mode de réalisation préféré de ladite composition, les pourcentages des substances actives individuelles par rapport à la somme des pourcentages de toutes les substances actives sont d'environ 50 % en poids de L-lysine, d'environ 15 % en poids de vitamine C, d'environ 2 % en poids de zinc, d'environ 10 % en poids d'extrait de raisin et d'environ 23 % en poids d'extrait d'orange amère, tous les pourcentages des substances actives individuelles constituant 100 % en poids de toutes les substances actives.
EP20797888.3A 2019-09-25 2020-09-24 Composition d'un complément alimentaire et/ou d'un additif nutritionnel pour aliments, forme posologique unitaire de ladite composition, et leur utilisation pour l'amélioration de la qualité de performance visuelle, y compris la sensibilité de contraste chez des personnes ayant besoin d'une telle amélioration, y compris des personnes souffrant d'au moins une maladie oculaire, en particulier le corps flottant du vitré Pending EP4033921A1 (fr)

Applications Claiming Priority (2)

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PL431268A PL431268A1 (pl) 2019-09-25 2019-09-25 Kompozycja suplementu diety i/lub dodatku odżywczego do żywności, jednostkowa postać dawkowania tej kompozycji i ich zastosowanie do poprawy jakości widzenia w tym wrażliwości na kontrast u osób potrzebujących takiej poprawy, w tym osób cierpiących na co najmniej jedną chorobę oczu, zwłaszcza na męty szklistkowe
PCT/PL2020/050069 WO2021061000A1 (fr) 2019-09-25 2020-09-24 Composition d'un complément alimentaire et/ou d'un additif nutritionnel pour aliments, forme posologique unitaire de ladite composition, et leur utilisation pour l'amélioration de la qualité de performance visuelle, y compris la sensibilité de contraste chez des personnes ayant besoin d'une telle amélioration, y compris des personnes souffrant d'au moins une maladie oculaire, en particulier le corps flottant du vitré

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US20080038367A1 (en) * 2006-08-11 2008-02-14 Sal Saloum Nutritional supplement compositions and methods of preparing
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US20110142766A1 (en) * 2009-12-16 2011-06-16 Sal Rafanelli Effervescent Multi-Vitamin Formulation and Methods of Use Thereof
CN101843784A (zh) * 2010-02-08 2010-09-29 崔晓廷 一种强效保护视力的多维叶黄素制剂
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PL431268A1 (pl) 2021-04-06
CA3151619A1 (fr) 2021-04-01
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CN114513971A (zh) 2022-05-17

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